Dipeptide-based prodrug linkers for aliphatic amine-containing drugs
    7.
    发明授权
    Dipeptide-based prodrug linkers for aliphatic amine-containing drugs 有权
    用于脂肪族胺的药物的基于二肽的前药接头

    公开(公告)号:US09062094B2

    公开(公告)日:2015-06-23

    申请号:US13574092

    申请日:2011-01-21

    摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aliphatic amine group is conjugated to one or more polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

    摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含药物接头缀合物DL,其中D是含有脂族胺基团的生物活性部分通过含二肽的接头L与一个或多个聚合物载体缀合。这种载体 连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。

    Carrier-linked carbamate prodrug linkers
    9.
    发明授权
    Carrier-linked carbamate prodrug linkers 有权
    载体连接的氨基甲酸酯前药接头

    公开(公告)号:US09561285B2

    公开(公告)日:2017-02-07

    申请号:US13574120

    申请日:2011-01-21

    IPC分类号: A61K47/48

    摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

    摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含药物连接物缀合物DL,其中D是含有芳族羟基的生物活性部分,通过含有次氨基甲酸酯的接头L与一个或多个聚合物载体缀合。 载体连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。

    CARRIER-LINKED CARBAMATE PRODRUG LINKERS
    10.
    发明申请
    CARRIER-LINKED CARBAMATE PRODRUG LINKERS 有权
    携带链接的碳酸氢钠原料连接器

    公开(公告)号:US20130035635A1

    公开(公告)日:2013-02-07

    申请号:US13574120

    申请日:2011-01-21

    摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof, comprising a drug linker conjugate D-L, wherein D being a biologically active moiety containing an aromatic hydroxyl group is conjugated to one or more polymeric carriers via secondary carbamate-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeutically useful half-lives. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.

    摘要翻译: 本发明涉及其前体药物或其药学上可接受的盐,其包含药物连接物缀合物DL,其中D是含有芳族羟基的生物活性部分,通过含有次氨基甲酸酯的接头L与一个或多个聚合物载体缀合。 载体连接的前药实现具有治疗有用的半衰期的药物释放。 本发明还涉及包含所述前体药物及其用作药物的药物组合物。